Assay Detail
Binding
CHEMBL2019815
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Displacement of [3H]-cAMP from human recombinant PDE7A
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
High affinity 3',5'-cyclic-AMP phosphodiesterase 7A (CHEMBL3012) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Isothiazole and isoxazole fused pyrimidones as PDE7 inhibitors: SAR and pharmacokinetic evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 7.64 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2019020 | — | — | 1 | 8.89 |
| CHEMBL2019104 | — | — | 1 | 8.40 |
| CHEMBL2019109 | — | — | 1 | 8.15 |
| CHEMBL2019106 | — | — | 1 | 8.10 |
| CHEMBL2019103 | — | — | 1 | 8.05 |
| CHEMBL2019108 | — | — | 1 | 7.96 |
| CHEMBL2019125 | — | — | 1 | 7.92 |
| CHEMBL2019113 | — | — | 1 | 7.92 |
| CHEMBL2019021 | — | — | 1 | 7.85 |
| CHEMBL2019134 | — | — | 1 | 7.85 |
| CHEMBL2019122 | — | — | 1 | 7.82 |
| CHEMBL2019110 | — | — | 1 | 7.80 |
| CHEMBL2019112 | — | — | 1 | 7.80 |
| CHEMBL2019123 | — | — | 1 | 7.77 |
| CHEMBL2019119 | — | — | 1 | 7.75 |
| CHEMBL2019107 | — | — | 1 | 7.75 |
| CHEMBL2019105 | — | — | 1 | 7.64 |
| CHEMBL2019124 | — | — | 1 | 7.60 |
| CHEMBL2019132 | — | — | 1 | 7.52 |
| CHEMBL2019135 | — | — | 1 | 7.51 |
| CHEMBL2019120 | — | — | 1 | 7.46 |
| CHEMBL2019111 | — | — | 1 | 7.46 |
| CHEMBL2019121 | — | — | 1 | 7.42 |
| CHEMBL2019128 | — | — | 1 | 7.41 |
| CHEMBL2019133 | — | — | 1 | 7.34 |
| CHEMBL2019102 | — | — | 1 | 7.34 |
| CHEMBL2019118 | — | — | 1 | 7.33 |
| CHEMBL2019114 | — | — | 1 | 7.18 |
| CHEMBL2019131 | — | — | 1 | 7.10 |
| CHEMBL2019115 | — | — | 1 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2019020 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL2019104 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2019109 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2019106 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2019103 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2019108 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2019125 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2019113 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2019021 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2019134 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2019122 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2019110 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2019112 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2019123 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2019107 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2019119 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2019105 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2019124 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2019132 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2019135 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL2019120 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2019111 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2019121 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2019128 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL2019133 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL2019102 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL2019118 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL2019114 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2019131 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2019115 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL2019126 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL2019116 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL2019117 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL2019127 | — | IC50 | - | — | - | |
| CHEMBL2019129 | — | IC50 | - | — | - | |
| CHEMBL2019130 | — | IC50 | - | — | - |